| Pyritinol Hydrochloride (Py-Hy) is the analogues of vitamin B6, it can treatAlzheimer,s disease in clinic. Its main products include Py-Hy tablet, Py-Hyinjection and Py-Hy producing needle. According to the clinical user feedback, theinjection has certain irritation. In order to avoid blood vessels excitant, on the basisof the predecessors,liposomes, this study prepared Py-Hy lipid nano-particles byPLGA as the carrier materials and the liposome of Py-Hy, but the drug loading ofPLGA nano-particles is very low, and the drug loading of liposomes is increased,the encapsulation rate is slightly increased and the irritation is reduced.This research study before prescribing of Py-Hy, determine the UV absorptionwavelength, Py-Hy was established by HPLC in vitro analysis method andultraviolet spectrophotometry, Also measured the oil-water partition coefficient ofPy-Hy, Py-Hy and cholesterol,Py-Hy and Cholesterol sodium sulfate, it showscholesterol sodium sulfate can improve the oil-water partition coefficient ofpyritinol hydrochloride, it provides reference for selected film flow regulator.In this study, the preparation process of PLGA lipid nano-particles andprescription screening was investigated, but the results show its drug loading isvery low, it has no practical value, so it is gave up. On the basis of predecessors,research, this study prepared Py-Hy liposomes by thin-film dispersion. Andevaluate and optimize its technology. Preparation process is mainly on theselection of solvent, temperature, the speed of film forming and ultrasonic, get theoptimal process. By using the single factor and orthogonal design method, theenvelopment rate of the liposome is as the main evaluation index, it inspected thescreening of the film used stabilizers, the type of phospholipids, the ionic strengthof hydration medium and the types of surfactants, the optimum prescription wasfinally determined.The optimal prescription and the preparation of the preparationshave been characterized. Finally the irritation of the liposome is evaluated throughthe animal model, it showed that the irritation is lower. hemolysis experiment iscarried and no hemolysis phenomenon happens. |